Lipid Nanoparticles: A Novel Approach for Brain Targeting

Shankar, Ravi; Joshi, Monika; Pathak, Kamla

doi:10.2174/2211738506666180611100416

Cited by 37 publications

(18 citation statements)

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“…Additionally, its oral bioavailability is of importance because chrysin has poor absorption with rapid metabolites elimination in the intestines 19 . Nevertheless, current technology that encompassed the use of nanoformulation (nanocapsule, nanoparticles), polymeric micelles, and liposomes that encapsulate chrysin may provide improvement in its BBB transmigration and bioavailability 49,50 . Moreover, the use of solid lipid nanoformulation was shown to increase in vitro drug release of chrysin to 83.19 % over 72 hours with a pattern biodistribution and stable physicochemical properties that supports the stability of chrysin (in an intact form) to penetrate the BBB 51 .…”

Section: Discussionmentioning

confidence: 99%

Chrysin Promotes Temozolomide-induced Apoptosis by Activating p38 MAPK and Suppressing Akt and ERK1/2 in Human Glioblastoma.

Kamarudin¹,

Parhar²

2021

Preprint

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Temozolomide (Tmz) faces the challenges of high chemoresistance and high dose leading to various side-effects. Chrysin exhibits anticancer and adjuvant effects in various cancer models. Nevertheless, chrysin’s synergistic effect with Tmz against Tmz-sensitive and Tmz-resistant human glioblastoma has never been reported. Chrysin and Tmz reduced the viability of A172 and LN18 in concentration- and time-dependent manner, with chrysin exhibited IC50 values lower than Tmz. The combination of chrysin and Tmz enhanced cell death (CI indexes between 0.59–0.98), suggesting synergistic efficacy of chrysin at lower concentrations. Chrysin promoted Tmz-induced phosphatidylserine externalization and depolarization of mitochondrial membrane potential. Chrysin promoted Tmz-induced suppression of pAkt (Ser473) and pERK1/2 (Thr202/Tyr204) while enhanced the phosphorylation of p38 MAPK (Thr180/Tyr182). This further reduced the antiapoptotic proteins (Bcl-2, Bcl-xL, Mcl-1), elevated proapoptotic proteins (Bax, Bad, Bak, PUMA, Noxa), and activated caspase-9 and caspase-3 compared to Tmz treatment alone. Pretreatment with Z-LEHD-FMK and Z-VAD-FMK attenuated apoptosis and restored caspase-9 and − 3 levels. However, pretreatment with Z-IETD-FMK did not suppress the promotion of apoptosis. Collectively, chrysin promotes Tmz-induced apoptosis through p38 MAPK activation and suppression of Akt and ERK1/2. These results suggest chrysin as a potential therapeutic adjuvant to improve Tmz effects in Tmz-sensitive and -resistant GBM.

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Section: Discussionmentioning

confidence: 99%

Chrysin Promotes Temozolomide-induced Apoptosis by Activating p38 MAPK and Suppressing Akt and ERK1/2 in Human Glioblastoma.

Kamarudin¹,

Parhar²

2021

Preprint

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“…Therefore, TfR were used to increase the uptake of SLN across the brain endothelial cells and also in brain tumor cells (Choudhury et al, 2018, Yang et al, 2008. SLN are the most promising carrier for the brain delivery of cytotoxic drugs due to its biocompatibility and biodegradability (Soni et al, 2017;Shankar et al, 2018). Doxorubicin (DOX) is a cytotoxic drug belongs to anthracycline class, shows a wide antitumor spectrum (Cagel et al, 2017, Cutts et al, 2005.…”

Section: Introductionmentioning

confidence: 99%

Transferrin anchored solid lipid nanoparticles for brain cancer treatment

Jain¹,

Soni²

2019

Asian J Pharm Pharmacol

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Objective: The aim of this study was to investigate the targeting potential of transferrin anchored solid lipid nanoparticles (SLN) loaded with doxorubicin (D-SLN-T).Transferrin receptors (TR) are Material and methods: highly expressed on blood brain barrier as well as brain cancer cells. Therefore, targeting TR using transferrin (Tf) improved the anticancer activity of prepared nanoparticles. The Tf coupled SLN were characterized by fourier transform infrared spectroscopy, transmission electron microscopy, particle size, particle size distribution, zeta potential, % entrapment efficiency, vitro drug release and cell line studies.The average Results and conclusion: particle size of the D-SLN-T was found to be 210.3±1.3 nm with a negative surface charge. The cell line studies, on U87 MG brain cancer cell lines, showed that the cytotoxicity of D-SLN-T was highly increased when anchored with transferrin. Also, the presence of transferrin on the surface of the D-SLN-T enhanced the cellular uptake of drug on U87MG cell line. The results of the cytotoxicity and cellular uptake studies clearly showed the potential of D-SLN-T in brain cancer treatment.

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“…Preclinical studies for Onpattro® most likely used MAR, as they contain data on intracellular radioactivity in hepatocytes, hepatic vascular cells (cell type not specified), and liver sinusoid lumen [22] . Obtaining cellular resolution has a more prominent role when cell-targeting moieties are used on LNPs, for example [71] , [72] , [73] , [74] , [75] , [76] . In this regard, MAR can sometimes (depending on reagent compatibility) be coupled to immunohistochemistry to verify targeted delivery [52] .…”

Section: Techniques Used For Authorized Rna Therapeuticsmentioning

confidence: 99%